Each mL contains: Ofloxacin 3 mg.
Pharmacology: The primary mechanism of action of ofloxacin appears to be the specific inhibition of DNA gyrase (topoisomerase II). This enzyme is responsible for the negative supercoiling of bacterial DNA and consequently for its topological configuration, governing functions such as RNA transcription, protein synthesis, DNA replication and repair functions.
Pharmacokinetics: Ofloxacin is rapidly and well absorbed from the gastrointestinal tract. Oral bioavailability is almost 100% and a peak plasma concentration of 3 to 5 micrograms/mL is achieved 1 to 2 hours after a dose of 400 mg by mouth. Absorption may be delayed by the presence of food, but the extent of absorption is not substantially affected. The plasma half-life ranges from 4 to 7 hours; in renal impairment values of 15 to 60 hours have been reported. About 25% is bound to plasma proteins. Ofloxacin is widely distributed in body fluids, including the CSF, and tissue penetration is good. It crosses the placenta and is distributed into breast milk. It also appears in the bile. There is limited metabolism to desmethyl and I-oxide metabolites; desmethylofloxacin has moderate antibacterial activity. Ofloxacin is eliminated mainly by the kidneys. Excretion is by tubular secretion and glomerular filtration and 65 to 80% of a dose is excreted unchanged in the urine over 24 to 48 hours, resulting in high urinary concentrations. Less than 5% is excreted in the urine as metabolites. From 4 to 8% of a dose may be excreted in the feces. Only small amounts of ofloxacin are removed by hemodialysis or peritoneal dialysis.
For the treatment of conjunctivitis and corneal ulcers caused by susceptible strains of the following bacteria: Gram-positive bacteria: S. aureus, S. epidermidis and S. pneumoniae. Gram-negative bacteria: H. influenzae.
Bacterial conjunctivitis: Days 1 and 2: Instill one (1) to two (2) drops every 2 to 4 hours in the affected eye(s).
Days 3 through 7: Instill one (1) to two (2) drops 4 times daily.
Bacterial corneal ulcer: Days 1 and 2: Instill one (1) to two (2) drops into the affected eye every 30 minutes while awake. Awaken at 4 and 6 hours after retiring and instill one (1) to two (2) drops.
Days 3 through 7 to 9: Instill one (1) to two (2) drops every hour while awake.
Days 7 to 9 through treatment completion: Instill one (1) to two (2) drops for 4 times daily.
Or as prescribed by the physician.
Discontinue medication if heavy or protracted use is suspected and flushes the eye with a topical ocular irrigant. In the event of accidental ingestion of 10 mL of ofloxacin ophthalmic solution although this amount may not be clinically significant in terms of overdosage, there could be an increased potential for systemic reactions.
Contraindicated in patients with hypersensitivity to the drug and to other quinolones or to any components of this product.
General: Prolonged use of ofloxacin ophthalmic solution may result in overgrowth of nonsusceptible organisms, including fungi.
Whenever clinical judgment dictates, the patient should be examined with the aid of magnification, such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.
In patients receiving systemic quinolone therapy, serious and occasionally fatal hypersensitivity (anaphylactic) reactions, some following the first dose, have been reported. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, tingling, angioedema (including laryngeal, pharyngeal or facial edema), airway obstruction, dyspnea, urticaria, and itching. Only a few patients had a history of hypersensitivity reactions. Serious anaphylactic reactions may require immediate emergency treatment with epinephrine.
Oxygen, I.V. steroids and airway management, including intubation, should be administered as clinically indicated.
The systemic administration of quinolones has led to lesions or erosions of the cartilage in weight-bearing joints and other signs of arthropathy in immature animals of various species. Ofloxacin, administered systemically at 10 mg/kg/day in young dogs (equivalent to 150 times the maximum recommended daily adult ophthalmic dose), has been associated with these types of effects.
Pregnancy: There have been no adequate and well-controlled studies performed in pregnant women. Since systemic quinolones have been shown to cause arthropathy in immature animals, ofloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Because ofloxacin taken systemically is excreted in breast milk, and there is potential for harm to nursing infants, a decision should be made whether to temporarily discontinue nursing during therapy or not to administer the drug, taking into account the importance of the drug to the mother.
Children: Safety and effectiveness of ofloxacin in infants below 1 year of age have not been established.
The most frequently reported drug-related adverse reaction was transient ocular burning or discomfort. Other reported reactions were ocular redness, stinging, itching, photophobia, tearing and dryness. One report of dizziness, one report of headache and one spontaneous report of toxic epidermal necrolysis have also been received.
As with all topical ophthalmic drugs, the potential exists for systemic effects. Ofloxacin used systemically has rarely been associated with serious side effects. Serious reactions reported for systemic dosing of ofloxacin include convulsions and increased intracranial pressure. For the oral dosage form of ofloxacin, gastrointestinal symptoms, mainly nausea/vomiting, pain/discomfort, diarrhea and anorexia, were reported most frequently, followed by CNS events (such as dizziness and headaches) and dermatological or hypersensitivity reactions. Photophobia was reported rarely in clinical trials with systemic ofloxacin and phototoxicity has been reported with other drugs in this class.
Specific drug interaction studies have not been conducted with ofloxacin ophthalmic solution. Interactions between ofloxacin and caffeine have not been detected. Systemic use of ofloxacin with nonsteroidal anti-inflammatory drugs has shown that the risk of CNS stimulation and convulsive seizures may increase. A pharmacokinetic study in 15 healthy males has shown that the steady-state peak theophylline concentration increased by an average of approximately 9% and the AUC increased by an average of approximately 13% when oral ofloxacin and theophylline were administered concurrently.
Store at temperatures not exceeding 30°C.
S01AE01 - ofloxacin ; Belongs to the class of quinolone antiinfectives. Used in the treatment of eye infections.
Ophth soln 0.3% w/v x 5 mL x 1's.